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以双氢青蒿素(DHA)为原料,与草酰氯发生酰化反应,然后经硫代吗啉取代反应、双氧水氧化反应得到青蒿砜1,由1经过烷基化反应、脱硅保护基和碘代反应得到青蒿砜-碘代物2α;以三乙胺为催化剂,2α与哌嗪类化合物、CS_2在“一锅煮”条件下得到青蒿砜-氨基二硫代甲酸酯化合物(3a~3d)。所有目标化合物的结构均经~1H NMR、~(13)C NMR、IR和HR-ESI-MS得到确证。
Using dihydroartemisinin (DHA) as the raw material, acylation reaction with oxalyl chloride is carried out, then thiomorpholine is substituted for the reaction, and the oxidative reaction of hydrogen peroxide is performed to obtain artesunate 1. After the alkylation reaction is carried out, the desilication protective group And iodine to obtain the artesunate sulfone-iodide 2α; using triethylamine as a catalyst, 2α and piperazine compounds, and CS_2 under a “one-pot” condition to obtain the artesunate sulfone-aminodithiocarboxylate compound 3a ~ 3d). The structures of all the target compounds were confirmed by ~ 1H NMR, ~ (13) C NMR, IR and HR-ESI-MS.